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Literature summary for 2.1.1.360 extracted from

  • Gao, Y.; Ge, W.
    The histone methyltransferase DOT1L inhibits osteoclastogenesis and protects against osteoporosis (2018), Cell Death Dis., 9, 33 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
EPZ004777 selective inhibitor Mus musculus
EPZ5676 selective inhibitor Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3 S-adenosyl-L-methionine + a [histone H3]-L-lysine79 Mus musculus overall reaction 3 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-L-lysine79 Mus musculus
-
S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-N6,N6-dimethyl-L-lysine79 Mus musculus
-
S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine79 Mus musculus
-
S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine79
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
macrophage
-
Mus musculus
-
RAW-264.7 cell
-
Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3 S-adenosyl-L-methionine + a [histone H3]-L-lysine79 overall reaction Mus musculus 3 S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-L-lysine79
-
Mus musculus S-adenosyl-L-homocysteine + a [histone H3]-N6-methyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-N6,N6-dimethyl-L-lysine79
-
Mus musculus S-adenosyl-L-homocysteine + a [histone H3]-N6,N6,N6-trimethyl-L-lysine79
-
?
S-adenosyl-L-methionine + a [histone H3]-N6-methyl-L-lysine79
-
Mus musculus S-adenosyl-L-homocysteine + a [histone H3]-N6,N6-dimethyl-L-lysine79
-
?

Synonyms

Synonyms Comment Organism
DOT1L
-
Mus musculus
H3K79 methyltransferase
-
Mus musculus

Expression

Organism Comment Expression
Mus musculus enzyme levels are upregulated during osteoclast differentiation up

General Information

General Information Comment Organism
malfunction enzyme knockdown enhances cell fusion and resorption activity in RAW264.7 osteoclastogenesis model. Enzyme inhibition enhances bone loss in ovariectomized mice Mus musculus
physiological function the enzyme inhibits osteoclastogenesis and protects against osteoporosis Mus musculus